6. aminoglycosides

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6. aminoglycosides

  1. 1. Aminoglycosides Tetra cyclines Macrolids Chloramphenicol
  2. 2.  Structure Glycosidic Aminosugar - O - Aminocyclitol 2-deoxystreptamine - O- Aminosugar Streptomycin Streptidine - O - Strepose aminosugar - O - N-methyl-Lglucosamine aminosugar Streptobiosamine
  3. 3. Aminoglycosides Penetrate Bact. Cell Wall To Periplasmic Space Transport Across Cytoplasmic Membrane (Oxygen Dependent) Bind To 30s Ribosomal Units Prevent Formation of ‘Initiation Complex’ Misreading of Genetic Code on mRNA Incorrect Amino Acids into Peptide Chain Inhibits Protein Synthesis
  4. 4.  All derived from an actinomycete or are semisynthetic derivatives  Bactericidal  Are  action highly polar compounds GIT poor absorption so IV/IM  More active in alkaline pH
  5. 5. • STREPTOMYCIN (1944) • KANAMYCIN (1957 ) • GENTAMICIN (1964) • AMIKACIN • SISOMICIN • NEOMYCIN • NEITILMICIN • FRAMYCETIN • TOBRAMYCIN 1967
  6. 6.  Suffix-“Mycin”- Streptomyces  “Micin’-Micromonospora
  7. 7.  Half life 1-3hr.  Concentration  Single depended killing daily dose result in higher tissue concentration  Interval 8-12hr
  8. 8. 1. Plasmid Mediated Bacterial Transferase Enzymes 2. Deletion of Porin Channels 3. Alteration of Receptor Protein on 30s Ribosomal Unit
  9. 9. • Very Poor Oral Bioavailability • Poor Distribution • Do Not Cross BBB • Excreted Through Kidney • Excretion is directly proportion to creatine clearence
  10. 10. • AEROBIC G-ve BACILLI • ENTEROBACTERIACEAE • NOT EFFECTIVE AGAINST : G +ve BACILLI G –ve COCCI ANAEROBES
  11. 11. OTOTOXICITY:AG causes impairment of 8th cranial nerve., accumulate in the endolymph and perilymph of the inner ear leading to vestibular and cochlear damage. • Irrversible NEUROMUSCULAR BLOCKADE
  12. 12. NEPHROTOXICITY Inhibition of intracellular Phospholipase A2 in renal brush border Leads to lysosomal distension ,rapture Release acid hydrolases & AG Free drug binds to other cellular organelles Leading to degeneration and necrosis
  13. 13.  Spectrum : Y. Pestis, Brucella, F.Tularensis, M.Tuberculosis   TOXICITY : Vestibular > Auditory Lowest Nephrotoxicity USES : • • • • Tuberculosis SABE Plague Tularemia & Brucellosis
  14. 14.    Spectrum : Pseudomonas, Proteus, E. Coli, Klebsiella, Enterobacteria & Seretia. TOXICITY : More Nephrotoxic USES : • Respiratory Infection in Critically Ill Pt. • Pelvic Infection • SABE • UTIs • Pseudomonal Infections • Infected Wounds, Burns, & Conjunctivitis
  15. 15.  Clinically & PK similar to Gentamicin  Susceptible to Aminoglycoside Inactivating Enzymes  Used Interchangeably with Gentamicin
  16. 16.  Semi synthetic Derivative of SISOMYCIN  Resistant to Inactivating Enzymes  Lesser Ototoxicity  Used in Gentamicin Resistant Infections
  17. 17.  Identical To Gentamicin  2-4 times More Active Against Pseudomonas & Proteus  Ototoxicity & Nephrotoxicity < Gentamicin  Reserve Alternative to ‘G’
  18. 18.  RESISTANT TO BACTERIAL ENZYMES  USED against Gentamicin & Tobramycin Resistant Infections  USES: • Multi drug Resistant TB • Hospital Acquired Infections  Hearing loss > Vestibular loss
  19. 19.  HIGHLY TOXIC  UESE • Infected Wounds, Ulcers, Burn • External Ear & Eye Infections • Preoperative Intestinal Antiseptic • Hepatic Coma

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